A combined targeted/phenotypic approach for the rapid identification of novel antiangiogenics with in vivo efficacy is herein reported. Considering the important role played by the tyrosine kinase c-Src in the regulation of tumour angiogenesis, we submitted our in-house library of c-Src inhibitors to a sequential screening approach: in silico screening on VEGFR2, in vitro screening on HUVEC cells, ADME profiling, formulation and in vivo testing on a zebrafish model. A promising antiangiogenic candidate able to interfere with the vascular growth of a zebrafish model at low micromolar concentration was thus identified.

Botta, M., Evensen, L., Dreassi, E., Zamperini, C., Caporicci, M., Falchi, F., et al. (2012). A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model:from in silico screening to cyclodextrin formulation. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 22, 5579-5583 [10.1016/j.bmcl.2012.07.014].

A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model:from in silico screening to cyclodextrin formulation

BOTTA, MAURIZIO;DREASSI, ELENA;ZAMPERINI, CLAUDIO;FALCHI, FEDERICO;
2012-01-01

Abstract

A combined targeted/phenotypic approach for the rapid identification of novel antiangiogenics with in vivo efficacy is herein reported. Considering the important role played by the tyrosine kinase c-Src in the regulation of tumour angiogenesis, we submitted our in-house library of c-Src inhibitors to a sequential screening approach: in silico screening on VEGFR2, in vitro screening on HUVEC cells, ADME profiling, formulation and in vivo testing on a zebrafish model. A promising antiangiogenic candidate able to interfere with the vascular growth of a zebrafish model at low micromolar concentration was thus identified.
2012
Botta, M., Evensen, L., Dreassi, E., Zamperini, C., Caporicci, M., Falchi, F., et al. (2012). A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model:from in silico screening to cyclodextrin formulation. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 22, 5579-5583 [10.1016/j.bmcl.2012.07.014].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/40376
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